scholarly journals Qualitative Portrayal of Esomeprazole Magnesium by Exploring Diverse Analytical and Investigative Approaches

2021 ◽  
pp. 52-68
Author(s):  
Kapil Kanwar ◽  
Surya Prakash Gautam
Keyword(s):  
Phosphate Buffer ◽  
Water Solubility ◽  
Uv Spectroscopy ◽  
Angle Of Repose ◽  
Simulated Gastric Fluid ◽  
Log P ◽  
P Value ◽  
Distilled Water ◽  
Simulated Intestinal Fluid ◽  
Esomeprazole Magnesium

Purpose: The present study was intended to qualitatively analyze and drive meaningful statistics for Esomeprazole magnesium; to establish its inherent properties qualitatively & quantitatively. Methods: Esomeprazole magnesium was analyzed using various traditional & modern analytical and investigative tools viz FTIR, HPLC, UV spectroscopy, X-ray diffraction, zetasizer. Results: The absorption maxima were found at 301 nm with UV Spectrophotometric and HPLC analysis. The particle size of the drug was analyzed through Malvern zetasizer employing water as diluent and found to be 11.818 µm. The quantitative solubility of Esomeprazole magnesium was predicted in various solvents at 25 0C and found that it was most soluble in methanol and was least soluble in distilled water. Solubility was also found to be pH-dependent. Solubility increases with an increase in pH. The order of solubility determined was; Methanol (1.214 mg/ml) > Phosphate buffer pH- 7.4 (0.521 mg/ml) > Simulated Intestinal fluid pH-6.8 (0.475 mg/ml) > Phosphate buffer pH- 6.8 (0.466 mg/ml) > Simulated Gastric fluid pH-1.2 (0.147 mg/ml) > 0.1 N HCl (0.131 mg/ml) > Distilled water (0.017 mg/ml). The predicted log P value was found to be 2.39. Conclusion: Esomeprazole magnesium was qualitatively analyzed using various analytical techniques to establish its inherent properties quantitatively. It is an off-white amorphous powder with a characteristic obnoxious odor and slightly bitter taste. The drug was identified through FTIR, using the classification of characteristic peaks of functional groups in the spectrum and also additionally through analytical methods viz HPLC, UV spectroscopy and found the absorption maxima at 301 nm. The linear regression analyses of a standard plot from UV spectrophotometric analysis demonstrate an unswerving relationship in the concentration range of 5-30μg/ml. The log P value indicates that the drug is significantly lipophilic. Various Micromeritic parameters like the Angle of repose, compressibility index, and Hausner's ratio predict the inherent flow properties of Esomeprazole magnesium as Fair (aid not needed). The present study will be an asset in the development of a modified released quick action formulation (Tablet-in-Tablet), to offer quick and protracted relief in gastritis and allied disorders.

scholarly journals A Comparison of Solubility, Stability, and Bioavailability between Astilbin and Neoastilbin Isolated from Smilax glabra Rhizoma

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4728
Author(s):  
Dan Zheng ◽  
Yi-Ting Ruan ◽  
Zhong-Ping Yin ◽  
Qing-Feng Zhang
Keyword(s):  
Water Distribution ◽  
Water Solubility ◽  
Gastric Fluid ◽  
Hplc Method ◽  
Absolute Bioavailability ◽  
Simulated Gastric Fluid ◽  
Log P ◽  
Simulated Intestinal Fluid ◽  
Significant Difference ◽  
Oil Water

Astilbin and neoastilbin are two flavonoid stereoisomers. In the present study, their solubility, stability, and bioavailability were compared in a rat. The results revealed that the water solubility of astilbin and neoastilbin was 132.72 μg/mL and 217.16 μg/mL, respectively. The oil–water distribution coefficient (log P) of astilbin and neoastilbin in simulated gastric fluid (SGF) was 1.57 and 1.39, and in simulated intestinal fluid (SIF) was 1.09 and 0.98, respectively. In SIF, about 78.6% astilbin remained after 4 h of incubation at 37 °C, while this value was 88.3% for neoastilbin. Most of the degraded astilbin and neoastilbin were isomerized into their cis-trans-isomer, namely neoisoastilbin and isoastilbin, respectively, and the decomposed parts were rare. For bioavailability comparison in a rat, an HPLC method for trace amounts of astilbin and neoastilbin determination in plasma was developed, and the pretreatment of plasma was optimized. A pharmacokinetic study showed that the absolute bioavailability of astilbin and neoastilbin in a rat showed no significant difference with values of 0.30% and 0.28%, respectively.

PHYSICOCHEMICAL PROPERTIES DETERMINATION OF PICROSIDE-II

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (08) ◽  
pp. 27-37
Author(s):  
S. Bhusari ◽  
A Chaudhary ◽  
G Shrangare ◽  
M. Rindhe ◽  
P. Wakte ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Linseed Oil ◽  
Angle Of Repose ◽  
Log P ◽  
P Value ◽  
Solubility Study ◽  
Picroside Ii ◽  
Compressibility Index ◽  
Pka Determination

The aim of the present study is to determine the physicochemical properties of Picroside-II, a phytochemical obtained from the herb of Picrorhiza kurroa. The solubility study of picroside-II shows that it has better solubility in water up to 2.46 mg/mL than organic solvents. The solubility of picroside-II in linseed oil was found to be 71.46 mg/mL. The solubility of Picroside-II in surfactant like Transcutol P and labrasol was found to be 907.80 and 535.90 mg/mL, respectively. Picroside-II had a melting point in the range of 130 to 135°C. The log P value of picroside-II was estimated using shake flask method followed by UV analysis. The log P value of picroside-II was found to be -0.09675, which shows its hydrophilicity. The pKa determination of picroside-II was carried out by using UV-visible spectrophotometer and the pKa value was found to be 7.80. The particle size distribution of picroside-II powder was also carried out and the maximum particles of picroside-II are in the range of 53-75 μm. Flow properties of picroside-II were also studied. bulk and tapped density of picroside-II powder was found to be 0.149 and 0.248, respectively. The Hausner ratio and compressibility index were also calculated and it was found to be 1.66 and 39.99, which confirm the poor flow properities of picroside-II powder. The angle of repose of picroside-II was found to be 41.08°, which shows the passable flow of picroside-II. Water was found to be the better extractive solvent for picroside-II; the extractive value of picroside-II in water was found to be 9.12%.

scholarly journals DEVELOPMENT OF LIQUISOLID FORMULATION FOR IMPROVED SUSTAINED RELEASE OF PROPRANOLOL HYDROCHLORIDE

2021 ◽  
pp. 210-216
Author(s):  
ALIYAH ALIYAH ◽  
EMILIA UTOMO ◽  
ANDI DIAN PERMANA ◽  
ERNAWATI
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Propylene Glycol ◽  
Gastric Fluid ◽  
Angle Of Repose ◽  
Simulated Gastric Fluid ◽  
Polysorbate 80 ◽  
Propranolol Hydrochloride ◽  
Coating Materials ◽  
Simulated Intestinal Fluid

Objective: The aim of this study was to develop a liquisolid formulation of propranolol hydrochloride to obtain an improved sustained release profile by varying the ratio of liquid vehicles. Methods: In this study, propranolol hydrochloride (PPH) was dispersed in the combination of propylene glycol and polysorbate 80, as the liquid vehicles, with different ratios. Eudragit® RL and Aerosil® were used as carrier and coating materials, respectively, to produce a dry and free-flowing powder. In addition, HPMC was used to amplify the retardation effect. The prepared formulations were evaluated for its physicochemical properties, including loss on drying, flow rate, angle of repose calculation, drug content analysis, FT-IR spectroscopy, as well as dissolution studies. The obtained dissolution profiles were subsequently fitted to the mathematical model in order to determine the drug kinetics. Results: The results show that all formulations performed dry and free-flowing granules containing PPH in the range of 7-9%. Furthermore, all the prepared formulations were able to sustain the drug release for a total of 8 h in two different dissolution media, namely simulated gastric fluid and simulated intestinal fluid. F4 containing propylene glycol and polysorbate 80 (1:2) possessed the lowest drug release rate. It was also obtained that F1 and F3 followed first-order kinetics while F2, F4, and F5 complied with the Higuchi model. Conclusion: Overall, there was no difference in all the dissolution profiles based on the calculation of the difference and similarities factor.

A Review on Recent Controlled Release Strategies for Oral Drug Delivery of Repaglinide (a BCS Class II Drug)

2021 ◽  
Vol 10 ◽  
Author(s):  
Saba Albetawi ◽  
Amer Abdalhafez ◽  
Ala Abu-Zaid
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Pancreatic Beta Cells ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Oral Drug ◽  
Log P ◽  
P Value

: Repaglinide is an antidiabetic drug that works by stimulating insulin secretion from pancreatic beta cells. Repaglinide is practically insoluble in water with a water solubility of 34 µg/mL at 37 ˚C, and it has a high absorption rate from the gastrointestinal tract following oral administration since the log P value of repaglinide is 3.97. The low aqueous solubility and the high permeability of repaglinide represent a typical behavior for drugs that belong to class II Biopharmaceutical Classification System (BCS II). Managing type-2 diabetes mellitus with repaglinide is considered a burdensome therapy, as it requires frequent dosing of repaglinide before each meal to maintain its therapeutic plasma concentration due to its short plasma half-life of approximately one hour. Hence the present review aims to discuss thoroughly the various approaches investigated in recent years to develop drug delivery systems that improve oral delivery of repaglinide, including nanoemulsions, solid lipid nanoparticles, nanostructured lipid carriers, sustained-release hydrophilic matrix, floating microspheres, and nanocomposites.

scholarly journals Formulation and development of Serratiopeptidase enteric coated tablets and analytical method validation by UV Spectroscopy

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Vijay Kumar Panthi ◽  
Saurav Kumar Jha ◽  
Raghvendra Chaubey ◽  
Rudra Pangeni
Keyword(s):  
Drug Release ◽  
Analytical Method ◽  
Uv Spectroscopy ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Simulated Intestinal Fluid ◽  
Analytical Method Validation ◽  
Analytical Technique ◽  
Enteric Coated

Serratiopeptidase (SRP) is a proteolytic enzyme that emerged as one of the most potent anti-inflammatory and analgesic drugs. The purpose of the present study was to formulate and evaluate enteric-coated tablets for SRP and investigate their stability using a simple and validated analytical method by ultraviolet (UV) spectroscopy. The colloidal silicon dioxide (2.50%), sodium starch glycolate (3.44%), and crospovidone (2.50%) were used as appropriate excipients for the development of core part of tablets. To protect the prepared tablets from acidic environment in the stomach, white shellac, castor oil, HPMC phthalate 40, and ethyl cellulose were used. The seal coating and enteric coating attained were 2.75% and 6.74%, respectively. SRP was found to be linear at 265 nm in the concentration range of 25–150 µg/mL. The results revealed that our developed method was linear (R2 = 0.999), precise (RSD % = 0.133), and accurate (% recovery = 99.96–103.34). The formulated SRP tablets were found to be stable under accelerated conditions as well as under room temperature for 6 months (assay %: >97.5%). The in vitro drug release study demonstrated that enteric-coated tablets were able to restrict SRP release in both acidic environments: 0.1 N HCl and simulated gastric fluid (pH 1.2). Moreover, at 60 minutes, the formulated SRP tablets revealed 13.0% and 8.98% higher drug release in phosphate buffer (pH 6.8) and simulated intestinal fluid (pH 6.8), respectively, compared to the marketed tablet formulation. This study concludes that enteric-coated tablets of SRP with higher drug release in the intestine can be prepared and examined for their stability using validated analytical technique of UV spectroscopy.

Freeze-fracture, freeze-etch complementary pairs of virus-infected cells reveal value of etching even when relatively high concentrations of cryoprotectants are used

1978 ◽  
Vol 36 (2) ◽  
pp. 136-137
Author(s):  
Russell L. Steere ◽  
Eric F. Erbe
Keyword(s):  
Plant Tissue ◽  
Phosphate Buffer ◽  
Infected Plant ◽  
Freeze Fracture ◽  
Distilled Water ◽  
Virus Infected Plant ◽  
Infected Cells ◽  
High Concentrations

It has been assumed by many involved in freeze-etch or freeze-fracture studies that it would be useless to etch specimens which were cryoprotected by more than 15% glycerol. We presumed that the amount of cryoprotective material exposed at the surface would serve as a contaminating layer and prevent the visualization of fine details. Recent unexpected freeze-etch results indicated that it would be useful to compare complementary replicas in which one-half of the frozen-fractured specimen would be shadowed and replicated immediately after fracturing whereas the complement would be etched at -98°C for 1 to 10 minutes before being shadowed and replicated.Standard complementary replica holders (Steere, 1973) with hinges removed were used for this study. Specimens consisting of unfixed virus-infected plant tissue infiltrated with 0.05 M phosphate buffer or distilled water were used without cryoprotectant. Some were permitted to settle through gradients to the desired concentrations of different cryoprotectants.

PENENTUAN NILAI PARAMETER LIPOFILITAS SENYAWA 4-KLOROBENZOILTIOUREA DAN UJI POTENSIASI TERHADAP TIOPENTAL PADA MENCIT PUTIH (Mus musculus)

2019 ◽  
Vol 4 (1) ◽  
pp. 1
Author(s):  
Dini Kesuma
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Electronic Properties ◽  
Mus Musculus ◽  
Log P ◽  
P Value ◽  
Lead Compounds ◽  
Significant Difference ◽  
Central Nervous System Depressant ◽  
The Central Nervous System

Synthesis of the 4-chlorobenzoylthiourea compound was carried out by acylating thiourea with 4-chlorobenzoyl chloride. The 4-chlorobenzoylthiourea compound  will increase the lipophilic and the electronic properties other than the lead compounds of benzoylthiourea in order to, by expectation, raise the central nervous system depressant as well. The lipophilic would affect the ability of the compounds in penetrating biological membranes, which is highly dependent on the solubility of the drug within lipid/water. Log P is the most common method used in determining the parameter value. This experiment was to mix two dissolvents (octanol and water) which are immissible. The both levels of the compounds were carefully observed by a spectrophotometer UV-Vis. From the test, the result of log P value of the 4-chlorobenzoylthiourea compound was 2.32, while the theoretical log P value of the compounds, by using the π Hansch-Fujita method is 1.62 and the f Rekker-Mannhold method is 2.225. Consequently, the result of the test shows that there is a significant difference between the progress experiment and both theoretical log P methods. Moreover, in the test of the central nervous system depressant through the potentiation test to thiopental using mice indicates that the 4-chlorobenzoylthiourea compound have potentiation effects to thiopental compared to the lead compounds of benzoylthiourea.

Solubility Enhancement of the Poorly Water-Soluble Antiulcer Drug Famotidine by Inclusion Complexation

2013 ◽  
Vol 6 (1) ◽  
pp. 1983-1989 ◽  
Author(s):  
Shabnam Ain ◽  
V Gupta ◽  
Babita K ◽  
Q Ain ◽  
J Dahiya
Keyword(s):  
Inclusion Complex ◽  
Dissolution Rate ◽  
Phosphate Buffer ◽  
Physical Mixture ◽  
Water Soluble ◽  
Molar Ratio ◽  
Phase Solubility ◽  
Distilled Water ◽  
Physicochemical Interaction ◽  
Mixture Phase

Aqueous solubility is a critical factor for optimum drug delivery. In the present study, we investigated the potential of drug-cyclodextrin complexation as an approach for improving the solubility and bioavailability of famotidine, an H2-receptor antagonist and acid reducing drug which has poor solubility and bioavailability. Solubility improvement of drug by β-cyclodextrin was done by simple complexation approach using physical, kneading and co-precipitation methods and compared with physical mixture. Phase solubility profile indicated that the solubility of famotidine was significantly increased in presence of β-cyclodextrin and shows a linear graph with β-cyclodextrin indicating formation of inclusion complexes in a 1:1 molar ratio. β-Cyclodextrin-famotidine mixture have maximum stability constant 1477.6 M-1. The inclusion complex ratio 1:1 of kneading mixture was selected based on drug release profile and compared with physical mixture. Further characterization was done by  using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM) to identify the physicochemical interaction between drug and carrier and its effect on dissolution. Dissolution rate studies for selected inclusion complex was performed in 0.1 N HCl (pH 1.2), phosphate buffer (pH 7.5) and distilled water (pH 6.8) and compared these to pure drug profile which was found to be 2.34 fold increase in distilled water, 1.83 fold in HCl and 2.01 fold in phosphate buffer (pH 7.5). These results suggest that the kneaded complex of famotidine with β-cyclodextrin as hydrophilic complexation agent can substantially enhance the solubility and dissolution rate. Such complex has promising potential to improve the bioavailability of famotidine.  

Quantitative Structure-Property Relationship (QSPR) Study of the Hydrophobicity of Phenols and 2-(Aryloxy-a-acetyl)-phenoxathiin Derivatives

2008 ◽  
Vol 59 (11) ◽  
Author(s):  
Adrian Beteringhe ◽  
Ana Cristina Radutiu ◽  
Titus Constantinescu ◽  
Luminita Patron ◽  
Alexandru T. Balaban
Keyword(s):  
Water Solubility ◽  
Molecular Descriptors ◽  
Log P ◽  
Structure Property ◽  
Substituted Phenols ◽  
Reverse Phase ◽  
Aromaticity Index ◽  
Structure Property Relationship ◽  
Layer Chromatography ◽  
Energy Of Formation

In a preceding study, the molecular hydrophobicity (RM0) was determined experimentally from reverse-phase thin-layer chromatography data for several substituted phenols and 2-(aryloxy-a-acetyl)-phenoxathiin derivatives, obtained from the corresponding phenoxides and 2-(a-bromoacetyl)-phenoxathiin. QSPR correlations for RM0 were explored using four calculated molecular descriptors: the water solubility parameter (log Sw), log P, the Gibbs energy of formation (DGf), and the aromaticity index (HOMA). Triparametric correlations do not improve substantially the biparametric correlation of RM0 in terms of log Sw and HOMA.

Application of 32 Full Factorial Design and Desirability Function for Optimizing The Manufacturing Process for Directly Compressible Multi-Functional Co-Processed Excipient

2020 ◽  
Vol 17 (6) ◽  
pp. 523-539
Author(s):  
Jalpa Patel ◽  
Dhaval Mori
Keyword(s):  
Factorial Design ◽  
Spray Drying ◽  
Desirability Function ◽  
Full Factorial Design ◽  
Angle Of Repose ◽  
P Value ◽  
Independent Variables ◽  
Full Factorial ◽  
32 Full Factorial Design ◽  
Response Variables

Background: Developing a new excipient and obtaining its market approval is an expensive, time-consuming and complex process. Compared to that, the co-processing of already approved excipients has emerged as a more attractive option for bringing better characteristic excipients to the market. The application of the Design of Experiments (DoE) approach for developing co-processed excipient can make the entire process cost-effective and rapid. Objective: The aim of the present investigation was to demonstrate the applicability of the DoE approach, especially 32 full factorial design, to develop a multi-functional co-processed excipient for the direct compression of model drug - cefixime trihydrate using spray drying technique. Methods: The preliminary studies proved the significant effect of atomization pressure (X1) and polymer ratio (microcrystalline cellulose: mannitol - X2) on critical product characteristics, so they were selected as independent variables. The angle of repose, Carr’s index, Hausner’s ratio, tensile strength and Kuno’s constant were selected as response variables. Result: The statistical analysis proved a significant effect of both independent variables on all response variables with a significant p-value < 0.05. The desirability function available in Design Expert 11® software was used to prepare and select the optimized batch. The prepared co-processed excipient had better compressibility than individual excipients and their physical mixture and was able to accommodate more than 40 percent drug without compromising the flow property and compressibility. Conclusion: The present investigation successfully proved the applicability of 32 full factorial design as an effective tool for optimizing the spray drying process to prepare a multi-functional co-processed excipient.

Sign in / Sign up

Export Citation Format

Share Document